| 摘要 |
This patent describes the procedure closed to the separation of enantiomers 5-hetaryl-1,3,4,-thiadiaziones with a general formula (I), where R1 represent a residue with a general formula A; R2 and R3 individually always represent hydrogen or residue with a general formula A; R4 represents hydrogen, residue with a general formula A or acyl group with 1 up to 15 carbon atoms; A represents alkyl group with 1 up to 8 carbon atoms and n represents integer having a value 1, 2 or 3, based on kinetic splitting of racemate. This racemate closed compound with a general formula (I) is soluble in an inert solvent or in a mixture of solvents, the acylation with the use of chiral chloride of acid and the created diasteromeric mixture is undertaken to the reaction with amine. As result of that the total splitting of one diastereomer is done and the splitting of second one is very little, while the basic enatiomer is created. The splitting products are separated and the residual pure diasteromer is changed to the appropriate pure enatiomer based on the reaction with amine or alcohol.
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